ZA948285B - 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors - Google Patents

16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Info

Publication number
ZA948285B
ZA948285B ZA948205A ZA948205A ZA948285B ZA 948285 B ZA948285 B ZA 948285B ZA 948205 A ZA948205 A ZA 948205A ZA 948205 A ZA948205 A ZA 948205A ZA 948285 B ZA948285 B ZA 948285B
Authority
ZA
South Africa
Prior art keywords
inhibitors
androstane
aza
reductase
alpha
Prior art date
Application number
ZA948205A
Other languages
English (en)
Inventor
Philippe L Durette
William K Hagmann
Thomas J Lanza Jr
Soumya P Sahoo
Gary H Rasmusson
Richard L Tolman
Derek Von Langen
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of ZA948285B publication Critical patent/ZA948285B/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)
ZA948205A 1993-10-21 1994-10-21 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors ZA948285B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21

Publications (1)

Publication Number Publication Date
ZA948285B true ZA948285B (en) 1995-06-19

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA948205A ZA948285B (en) 1993-10-21 1994-10-21 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Country Status (29)

Country Link
US (4) US5739137A (fr)
EP (1) EP0724592B1 (fr)
JP (1) JP2862376B2 (fr)
KR (1) KR100363994B1 (fr)
CN (1) CN1058499C (fr)
AT (1) ATE175420T1 (fr)
BG (1) BG61978B1 (fr)
BR (2) BR9407866A (fr)
CA (1) CA2173863C (fr)
CY (1) CY2136B1 (fr)
CZ (1) CZ292614B6 (fr)
DE (1) DE69415824T2 (fr)
DK (1) DK0724592T3 (fr)
ES (1) ES2125495T3 (fr)
FI (1) FI961697A (fr)
HK (1) HK1009047A1 (fr)
HU (1) HUT74613A (fr)
IL (1) IL111357A (fr)
LV (2) LV11622B (fr)
NO (1) NO308037B1 (fr)
NZ (1) NZ275293A (fr)
PL (1) PL179611B1 (fr)
RO (1) RO116197B1 (fr)
RU (1) RU2142956C1 (fr)
SK (1) SK281645B6 (fr)
TW (1) TW413682B (fr)
UA (1) UA44257C2 (fr)
WO (1) WO1995011254A1 (fr)
ZA (1) ZA948285B (fr)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
WO1995011254A1 (fr) * 1993-10-21 1995-04-27 Merck & Co., Inc. INHIBITEURS DE L'ISOZYME 5α-REDUCTASE 1 DE 4-AZA-ANDROSTANE-5 A SUBSTITUTION EN POSITION 16
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
AU694576B2 (en) * 1994-10-21 1998-07-23 Merck & Co., Inc. Combination method for acne treatment
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
JPH11513684A (ja) * 1995-10-19 1999-11-24 メルク エンド カンパニー インコーポレーテッド １６−置換−６−アザ−ステロイド５α−レダクターゼ阻害剤
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US5945412A (en) * 1996-12-09 1999-08-31 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
EP1009740A1 (fr) * 1997-03-17 2000-06-21 Merck & Co., Inc. Methodes et compositions de traitement de la polykystose ovarienne
CA2308070A1 (fr) * 1997-10-28 1999-05-06 Merck & Co., Inc. Prevention de retention urinaire aigue precipitee
US6187925B1 (en) * 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
WO1999058550A1 (fr) * 1998-05-14 1999-11-18 Merck & Co., Inc. 7β-METHYL-16β-((4-METHYLSULFONYL)-PHENOXY)-4-AZA-5α-ANDROST-1-EN-3-ONE UTILISEE COMME INHIBITEUR D'ISO-ENZYME 5α-REDUCTASE 1
AR016257A1 (es) * 1998-05-14 2001-06-20 Merck & Co Inc Proceso para la sintesis estereoselectiva de ariloxi-4-aza-5alfa-androstan-3-onas, 16 alfa y 16 beta-sustituidas e insustituidas, e intermediariosobtenidos en dicho proceso.
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
AU754604B2 (en) * 1998-07-29 2002-11-21 Merck & Co., Inc. Tricyclic compounds
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
US20020198215A1 (en) * 2000-10-23 2002-12-26 Lino Tavares Terazosin transdermal device and methods
US20080125403A1 (en) * 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
JP2008534505A (ja) 2005-03-25 2008-08-28 メルク エンド カムパニー インコーポレーテッド テストステロンサプリメントおよび５アルファ−レダクターゼインヒビターによる男性の治療方法
US20060241696A1 (en) * 2005-04-26 2006-10-26 Stjepan Krco Method of limiting hair loss and promoting hair growth
FR2910002B1 (fr) * 2006-12-13 2009-01-30 Sanofi Aventis Sa Nouveau procede pour l'obtention diastereoselective d'une amine primaire chirale sur un steroide
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI593411B (zh) 2013-04-30 2017-08-01 徐懷山 組合物於製備抑制雄性素受體有關之功能及治療雄性素 受體相關之疾病的藥物之用途

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4220775A (en) * 1979-03-15 1980-09-02 Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
US4859681A (en) * 1984-02-27 1989-08-22 Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
US5120742A (en) * 1984-02-27 1992-06-09 Merck & Co., Inc. 17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-reductase inhibitors
US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α reductase inhibitors
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
DE3888378T2 (de) * 1987-04-03 1994-09-29 Merck & Co Inc Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen.
DE3888994T2 (de) * 1987-04-03 1994-11-03 Merck & Co Inc Behandlung von androgener Alopecia mit 17-beta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen.
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
CA2084798A1 (fr) * 1991-12-17 1993-06-18 Glenn J. Gormley Methode de prevention du carcinome prostatique a l'aide de 17beta -acyl -4-a-za-5.-androst-1-ene-3-ones
US5215894A (en) * 1992-02-25 1993-06-01 Merck & Co., Inc. Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors
GB2264494A (en) * 1992-02-25 1993-09-01 Merck & Co Inc 17b-n-monosubstituted carbamoyl-11-oxo-4-aza-5-a-androst-1-en-3-one testosterone-5-alpha reductase inhibitors
AU674145B2 (en) * 1992-05-20 1996-12-12 Merck & Co., Inc. New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
SK137994A3 (en) * 1992-05-20 1995-04-12 Merck & Co Inc 7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them
EP0641211A1 (fr) * 1992-05-21 1995-03-08 Endorecherche Inc. INHIBITEURS D'ACTIVITE DE LA TESTOSTERONE 5$g(a)-REDUCTASE
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
US5278159A (en) * 1992-10-06 1994-01-11 Merck & Co., Inc. Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors
US5380728A (en) * 1993-02-10 1995-01-10 Merck & Co., Inc. Aldehyde metabolite of 17β-N-monosubstituted-carbamoyl-4-aza-5α-a
US5407944A (en) * 1993-02-19 1995-04-18 Goldman; Boris E. Compositions and methods for promoting hair growth
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
WO1995011254A1 (fr) * 1993-10-21 1995-04-27 Merck & Co., Inc. INHIBITEURS DE L'ISOZYME 5α-REDUCTASE 1 DE 4-AZA-ANDROSTANE-5 A SUBSTITUTION EN POSITION 16
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
US5512555A (en) * 1994-07-21 1996-04-30 Merck & Co., Inc. Method of treating sweat-related conditions using finasteride, epristeride and a cholestan-3-one
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents

Also Published As

Publication number Publication date
PL179611B1 (pl) 2000-10-31
BG100516A (en) 1996-11-29
HUT74613A (en) 1997-01-28
FI961697A0 (fi) 1996-04-18
SK281645B6 (sk) 2001-06-11
US6204273B1 (en) 2001-03-20
IL111357A0 (en) 1994-12-29
LV12316B (en) 1999-11-20
EP0724592B1 (fr) 1999-01-07
AU8086194A (en) 1995-05-08
DK0724592T3 (da) 1999-08-30
CN1058499C (zh) 2000-11-15
HU9601037D0 (en) 1996-06-28
LV11622A (lv) 1996-12-20
FI961697A (fi) 1996-04-18
CA2173863C (fr) 2003-05-13
CY2136B1 (en) 2002-06-21
ATE175420T1 (de) 1999-01-15
UA44257C2 (uk) 2002-02-15
NO961575L (no) 1996-04-19
US5910497A (en) 1999-06-08
KR960705839A (ko) 1996-11-08
PL314039A1 (en) 1996-08-05
NO308037B1 (no) 2000-07-10
CZ292614B6 (cs) 2003-11-12
ES2125495T3 (es) 1999-03-01
BR1100217A (pt) 1999-11-09
BR9407866A (pt) 1996-10-29
JP2862376B2 (ja) 1999-03-03
DE69415824T2 (de) 1999-08-05
NO961575D0 (no) 1996-04-19
EP0724592A1 (fr) 1996-08-07
WO1995011254A1 (fr) 1995-04-27
IL111357A (en) 2001-01-28
NZ275293A (en) 1998-02-26
SK49696A3 (en) 1996-10-02
TW413682B (en) 2000-12-01
AU680063B2 (en) 1997-07-17
JPH09511213A (ja) 1997-11-11
CN1136318A (zh) 1996-11-20
CA2173863A1 (fr) 1995-04-27
KR100363994B1 (ko) 2003-04-10
LV11622B (en) 1997-06-20
RU2142956C1 (ru) 1999-12-20
HK1009047A1 (en) 1999-05-21
RO116197B1 (ro) 2000-11-30
US5739137A (en) 1998-04-14
CZ122896A3 (en) 1997-01-15
US5719158A (en) 1998-02-17
DE69415824D1 (de) 1999-02-18
LV12316A (lv) 1999-07-20
BG61978B1 (bg) 1998-11-30

Similar Documents

Publication Publication Date Title
HK1009047A1 (en) 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors
GEP20094660B (en) Pyran-2-ones and 5,6-dihydropyran-2-ones useful for treating hyperplasia and other diseases
EP0641208A4 (fr) INHIBITEURS DE 5--g(a)-REDUCTASE A BASE DE 4-AZASTEROIDES.
ATE143942T1 (de) Carbonsäurederivate als 5-alpha-reduktase- inhibitor
EP0748221A4 (fr) Derives de 4-aza-steroide substitue en position 7 utilises comme inhibiteurs de 5-alpha-reductase
CY2071B1 (en) Method of treating androgenic alopecia with 5-alpha reductase inhibitors
EP0649431A4 (en) 17-amino substituted 4-azasteroid 5-g(a)-reductase inhibitors.
EP0756481A4 (fr) DERIVES DU 17-g(b)-ARYLE-4-AZA-STEROIDE
EP0862556A4 (fr) Derives de steroides 17-alkyl-4-aza-7-substitues